1. Academic Validation
  2. Design and synthesis of novel 1,2,3-triazole-dithiocarbamate hybrids as potential anticancer agents

Design and synthesis of novel 1,2,3-triazole-dithiocarbamate hybrids as potential anticancer agents

  • Eur J Med Chem. 2013 Apr:62:11-9. doi: 10.1016/j.ejmech.2012.12.046.
Ying-Chao Duan 1 Yong-Cheng Ma En Zhang Xiao-Jing Shi Meng-Meng Wang Xian-Wei Ye Hong-Min Liu
Affiliations

Affiliation

  • 1 New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
Abstract

A series of novel 1,2,3-triazole-dithiocarbamate hybrids were designed, synthesized and evaluated for Anticancer activity against four selected human tumor cell lines (MGC-803, MCF-7, PC-3, EC-109). Majority of the synthesized compounds exhibited moderate to potent activity against MGC-803 and MCF-7. Among them, compounds 3a and 3c showed excellent broad spectrum Anticancer activity with IC50 values ranging from 0.73 to 11.61 μM and 0.49-12.45 μM, respectively. Particularly, compound 3a was more potent than 5-fluorouracil against all tested human Cancer cell lines. Flow cytometry analysis demonstrated that treatment of MGC-803 with 3c led to cell cycle arrest at G2/M phase accompanied by an increase in apoptotic cell death after 12 h.

Figures